62893-54-3Relevant articles and documents
New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-Butyl-2,3- dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: Variations at the 5 position
Janusz, John M.,Young, Patricia A.,Ridgeway, James M.,Scherz, Michael W.,Enzweiler, Kevin,Wu, Laurence I.,Gan, Lixian,Chen, Julian,Kellstein, David E.,Green, Shelley A.,Tulich, Jennifer L.,Rosario-Jansen, Theresa,Magrisso, I. Jack,Wehmeyer, Kenneth R.,Kuhlenbeck, Deborah L.,Eichhold, Thomas H.,Dobson, Roy L. M.
, p. 3515 - 3529 (1998)
We report an expansion of the scope of our initial discovery that 5- keto-substituted 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofurans (DHDMBFs) are antiinflammatory and analgesic agents. Several other functional groups have been introduced at the 5 position: amides, amidines, ureas, guanidines, amines, heterocycles, heteroaromatics, and heteroaryl ethenyl substituents in the 5 position all provide active compounds. These compounds are dual cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibitors. They inhibit both COX-1 and COX-2 with up to 33-fold selectivity for COX-2.
2-process for the preparation of cyclopropyl-ethylamine
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Paragraph 0044-0046, (2017/01/09)
The invention discloses a preparation method of 2-cyclopropyl ethylamine. The method includes the steps of A, compound 1 and nitromethane react under the action of alkali to obtain compound 2; B, the compound 2 is dehydrated under the action of dehydration reagent to obtain compound 3; C, the compound 3 reacts in solvent under the action of reducing agent to obtain compound 4; D, the compound 4 reacts under the action of reduction hydrogenation catalyst to obtain compound 5, namely the 2-cyclopropyl ethylamine. The preparation method has the advantages that operation conditions can be simplified, cost can be lowered, and easiness in large batch production is achieved. The synthesizing route is showed as follows.
NOVEL COMPOUNDS
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Page/Page column 19, (2015/03/04)
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, X, m, R2, Y, R3, Z, n, R4, A and B are as defined in the specification, processes for their prep